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拉替司汀及其衍生物的全合成及抗抑郁活性。

Total synthesis and antidepressant activities of laetispicine and its derivatives.

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.

出版信息

Molecules. 2012 Feb 3;17(2):1425-36. doi: 10.3390/molecules17021425.

DOI:10.3390/molecules17021425
PMID:22306832
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6268093/
Abstract

The first total synthesis of laetispicine (1a), an amide alkaloid isolated from the stems of Piper laetispicum C.DC (Piperaceae), and the synthesis of some of its derivatives were described. Based on the evaluation of antidepressant activities in the forced swimming test, compounds 1h and 1i were identified as potent and safe antidepressant lead compounds.

摘要

首次全合成了从 Piper laetispicum C.DC(胡椒科)茎中分离得到的酰胺生物碱 laetispicine(1a),并合成了一些衍生物。基于在强迫游泳试验中对抗抑郁活性的评估,化合物 1h 和 1i 被鉴定为具有潜力和安全的抗抑郁先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/3835621b54bb/molecules-17-01425-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/39a2b06264c7/molecules-17-01425-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/2b9aaf809cda/molecules-17-01425-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/7fcb67634f6f/molecules-17-01425-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/4412211fc152/molecules-17-01425-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/3835621b54bb/molecules-17-01425-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/39a2b06264c7/molecules-17-01425-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/2b9aaf809cda/molecules-17-01425-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/7fcb67634f6f/molecules-17-01425-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/4412211fc152/molecules-17-01425-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ffc/6268093/3835621b54bb/molecules-17-01425-g005.jpg

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本文引用的文献

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Phytomedicine. 2009 Sep;16(9):823-9. doi: 10.1016/j.phymed.2009.02.008. Epub 2009 May 15.
2
Bifunctional inhibitors of mevalonate kinase and mevalonate 5-diphosphate decarboxylase.甲羟戊酸激酶和甲羟戊酸5-二磷酸脱羧酶的双功能抑制剂。
Org Lett. 2006 Mar 16;8(6):1013-6. doi: 10.1021/ol052573s.
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Natural products to drugs: natural product derived compounds in clinical trials.
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Nat Prod Rep. 2005 Apr;22(2):162-95. doi: 10.1039/b402985m. Epub 2005 Mar 8.
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Novel cognitive improving and neuroprotective activities of Polygala tenuifolia Willdenow extract, BT-11.远志提取物BT-11的新型认知改善和神经保护活性
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